Bioorganic and Medicinal Chemistry Letters

, volume 20 , issue 19 , pages 5807-5810

Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors

Takumi Watanabe ¹

YOJI UMEZAWA ¹

Yoshikazu Takahashi ¹

Yuzuru AKAMATSU ¹

Hide authors affiliations Show authors affiliations: 1 affiliation

Institute of Microbial Chemistry, Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan |

Publication type: Journal Article

Publication date: 2010-10-01

Elsevier

Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

SJR: 0.472

CiteScore: 5.1

Impact factor: 2.2

ISSN: 0960894X, 14643405

DOI: 10.1016/j.bmcl.2010.07.131

Copy DOI

PubMed ID: 20728352

Organic Chemistry

Drug Discovery

Biochemistry

Molecular Biology

Pharmaceutical Science

Clinical Biochemistry

Molecular Medicine

Abstract

Pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase (OSC) inhibitors 3 and 4 were discovered by conducting a virtual screening, a docking study based on the crystallographic structure of OSC, and biological assays. The hit rate of the assays was increased by establishing appropriate substructural filters in the virtual screening stage. Amide derivatives of 8 and 12 preserved the inhibitory activity of parent compound 3, which provided a reasonable starting point for further structure-activity-relationship (SAR) studies on related compounds.

Found

1 citation

Larina Lyudmula

56 publications, 361 citations, 2 reviews

h-index: 10

A.E. Favorsky Irkutsk Institute of Chemistry of the Siberian Branch of the Russian Academy of Sciences

Photochemistry Center

Emanuel Institute of Biochemical Physics of the Russian Academy of Sciences

Chungnam National University

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GOST |

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GOST Copy

Watanabe T. et al. Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 19. pp. 5807-5810.

GOST all authors (up to 50) Copy

Watanabe T., UMEZAWA Y., Takahashi Y., AKAMATSU Y. Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 19. pp. 5807-5810.

RIS |

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RIS Copy

TY - JOUR

DO - 10.1016/j.bmcl.2010.07.131

UR - https://doi.org/10.1016/j.bmcl.2010.07.131

TI - Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors

T2 - Bioorganic and Medicinal Chemistry Letters

AU - Watanabe, Takumi

AU - UMEZAWA, YOJI

AU - Takahashi, Yoshikazu

AU - AKAMATSU, Yuzuru

PY - 2010

DA - 2010/10/01

PB - Elsevier

SP - 5807-5810

IS - 19

VL - 20

PMID - 20728352

SN - 0960-894X

SN - 1464-3405

ER -

BibTex |

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BibTex (up to 50 authors) Copy

@article{2010_Watanabe,

author = {Takumi Watanabe and YOJI UMEZAWA and Yoshikazu Takahashi and Yuzuru AKAMATSU},

title = {Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors},

journal = {Bioorganic and Medicinal Chemistry Letters},

year = {2010},

volume = {20},

publisher = {Elsevier},

month = {oct},

url = {https://doi.org/10.1016/j.bmcl.2010.07.131},

number = {19},

pages = {5807--5810},

doi = {10.1016/j.bmcl.2010.07.131}

}

MLA

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MLA Copy

Watanabe, Takumi, et al. “Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 19, Oct. 2010, pp. 5807-5810. https://doi.org/10.1016/j.bmcl.2010.07.131.

Publisher

Elsevier

Journal

Bioorganic and Medicinal Chemistry Letters

scimago Q2

wos Q2

SJR

0.472

CiteScore

5.1

Impact factor

2.2

ISSN

0960894X (Print)

14643405 (Electronic)